Bi-dentate compounds as kinase inhibitors

Chemistry: natural resins or derivatives; peptides or proteins; – Peptides of 3 to 100 amino acid residues – 8 to 10 amino acid residues in defined sequence

Reexamination Certificate

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C530S329000, C530S330000, C530S331000

Reexamination Certificate

active

07919581

ABSTRACT:
The present invention provides compound having the general structure A or pharmaceutically acceptable salts thereof:in-line-formulae description="In-line Formulae" end="lead"?Het-L-P  (A)in-line-formulae description="In-line Formulae" end="tail"?wherein Het is an aromatic moiety comprising a heterocyclic structure mimicking ATP, P is a docking site derived peptide or a docking site peptide mimetic, and L is a linking moiety, wherein L links the ATP mimetic to the docking site peptide moiety. The compounds having the general structure A can serve as inhibitors of kinases, such as the kinases JNK, Erk and p38.

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Salh. c-Jun N-terminal kinases as potential therapeutic targets. Review. Expert Opin. Ther. Targets. 2007. vol. 11, No. 10, pp. 1339-1353.
Barr et al. Identification of the Critical Features of a Small Peptide Inhibitor of JNK Activity. The Journal of Biological Chemistry. 2002, vol. 277, No. 13, pp. 10987-10997.

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